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VU0529331 

Cat. No. M28117
VU0529331  Structure
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Biological Activity

VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 µM and 5.2 µM for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.

Chemical Information
Molecular Weight 384.43
Formula C22H20N6O
CAS Number 1286725-49-2
Form Solid
Solubility (25°C) DMSO 5 mg/mL (Need ultrasonic and warming)
Storage Powder -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Meng Cui, et al. J Biol Chem. A novel small-molecule selective activator of homomeric GIRK4 channels

[2] Boris Shalomov, et al. J Physiol. A revised mechanism of action of hyperaldosteronism-linked mutations in cytosolic domains of GIRK4 (KCNJ5)

[3] Krystian A Kozek, et al. ACS Chem Neurosci. Discovery and Characterization of VU0529331, a Synthetic Small-Molecule Activator of Homomeric G Protein-Gated, Inwardly Rectifying, Potassium (GIRK) Channels

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Keywords: VU0529331  supplier, Potassium Channel, inhibitors, activators


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